Anti-lipolytic mechanisms of regulation include the binding of ABHD5 to
PLIN1 which is regulated allosterically by ABHD5-sensing of long-chain acyl-CoA
(LC-CoA). PNPLA2 hydrolytic activity can be inhibited by the interaction with
G0S2 which is independent of its interaction with ABHD5. In addition, PNPLA3 can
compete with PNPLA2 for binding to ABHD5, thereby sequestering ABHD5 away from
PNPLA2. PNPLA3 can also function to sequester fatty acids (FAs) through
lysophosphatidic acid acyltransferase or transacylase activity. LC-CoAs also
allosterically regulate the interaction between PNPLA3 and ABHD5. UBDX8 can bind
PNPLA2 to promote its segregation from the lipid droplet (LD) by VCP, followed
by ubiquitination (Ub) and elimination by the proteasome (26S). In the basal
state HSL is found mostly in the cytosol. Stimulatory signals lead to the
phosphorylation (P) of PLIN1 to release ABHD5 which can bind PNPLA2, and
phosphorylation of HSL promotes its trafficking to LDs and interaction with
PLIN1. This leads to the sequential hydrolysis of TAG by PNPLA2, hydrolysis of
DAG by HSL and hydrolysis of MAG by MGL to three FAs and glycerol. The
elimination of G0S2 and PNPLA3 by the ubiquitin-proteasome system (UPS), through
currently unknown mechanisms, would be pro-lipolytic.